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5-HTP and decarboxylase inhibitors

dopamimetic

Bluelighter
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Mar 21, 2013
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Are there any peripheral decarboxylase inhibitors (maybe naturally occurring ones) available besides carbidopa, which is only sold in combination with levodopa, to enhance the central availability of 5-HTP and reduce side effects of peripherally produced 5-HT like gastric disturbances...?

How much would such a combination enhance / potentiate the 5-HTP? (Edit: Its not dangerous even at 300mg 5-HTP with carbidopa, but this paper also does confirm that it'd be beneficial to combine.)
 
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There is talk that the active metabolite(produced from Microbiome in the intestines or possibly liver) of 5htp is the one that enters the CNS and causes neuroprotective effects(the carbon skeleton deaminated ).

The name of this is indole 3 propionic acid and it's in clinical trials under the name OXIGON for alzheimers disease.

So sorry 5htp probably won't enter the CNS at all very well like many believe. Very rate limited transporter unlike other amino acids. It's the carbon skeleton metabolite.

So the combination they speak of in the paper above is confusing as they try to correlate the whole neuroendocrine relationship to intake is not clear at all. Even if they took plasma levels of 5htp vs the hormones etc, I would be inclined to believe Caridopa is affecting the other metabolite in a way and their relationship is true. But the compounds are just mixed up.. I would try this but look into OXIGON.

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Zedsdead
 
That's new information, thanks!

So you'd say that 5-HTP does not enter the CNS at all, or just not readily? Levodopa is not very active on its own either when not taken in hefty doses or with carbidopa, cause of peripheral metabolism- thought this was by the same.

Since taking good doses of 5-HTP over the day definitely helps more than anything (besides of taking some SSRI of course) with SSRI discontinuation syndrome, brain zaps and all that. Just that it often leads to diarrhea and nausea.
 
5htp enters the CNS just not as readily and in concentration magnitude as smaller amino acids whose job are excitatory etc if you follow me.
Think of it as if many transporters exchange, concomitantly pump cations, glycine, gaba etc in a higher rate than tryptophan. Yes tryptophan/5htp enter the CNS but poorly.

Also consider the bioavailability of most amino acids are pretty piss poor (LOL WHAT??) No they actually are this is why we receive most of our amino acids in the form of peptides/proteins in the meats we eat. We hydrolyze these bonds and use this energy for transport etc. Just something to think about.
My suggestion? Does acetyl 5htp exist? Yes not super available and still many don't realize that all processes in the body are in multiple equilibriums and adding more of serotonin won't do much.

What we appear to be realizing is directed conduction of neuron systems is related to higher processing/etc. Neurotransmitters are kind of just like charge carriers (kinda but not really) a solid example of this is Modafinil and it's effects on gap junctions and the DAT..
ENDTANGENT
zedsdead
 
I always thought 5htp was essentially all decarboxylated outside of the BBB and the serotonin is destroyed by blood/tissue MAO before it can go anywhere.

See also, L-DOPA is not useful as a theraputic w/o peripheral amino acid decarboxylase inhibitors.

Indole-3-alkylcarboxylates are also plant growth horomones (auxins), are they not? How about indole-3-acetic acid? I wonder how much bioactivity you'd see from eating some young fresh shoots of e.g. bamboo...
 
This is all very true however no process is 100% absolute and whatever fraction makes it to the liver or eventually to the intestines can be modified possibly acylated and reabsorbed.

It's peculiar hydrocinnamic acid the carbon skeleton of phenylalanine is bricks and not worthwhile in the brain but apparently the metabolite 3-hydroxy cinnamic acid is possibly useful. (pure indole is not as well epoxidated to the hydroxy indole in the body I believe but if it is I would look at the 4/5 hydroxy indole propionic acids)

I would suggest :
Indole propionyl acetate
4-hydroxy/5-hydroxy indole propionyl acetate
3-hydroxy cinaminnyl acetate

For possible neuroprotective most likely (not true nootropic) agents
Zedsdead
 
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